Synthesis and characterization of quinazoline-cinnamic acid hybrid as Alzheimer's drug candidate

Other Title(s)

تشييد و تحليل مركب هجين من كوينازولين-سيناميك أسيد كعالج محتمل لمرض الزهايمر

Dissertant

al-Ẓalimi, Duha Muhsin Abd al-Husayn

Thesis advisor

Abu Diyyah, Zayd

University

Isra University

Faculty

Faculty of Pharmacy

University Country

Jordan

Degree

Master

Degree Date

2020

English Abstract

Alzheimer’s disease (AD) has been one of the most important cause of death for elderly people around the world.

It’s characterized by cognitive impairment and memory loss, mainly because of damage of cholinergic neurons in the fore-brain and hippocampus and reducing amount of Acetylcholine as well, the second main cause is the oxidative stress by reactive oxygen species (ROS) and reactive nitrogen species (RNS) in many brain region.

Current treatment available for this neurodegenerative disease was mainly symptomatic and they were not affected on disease progression.

Quinazoline moiety as promising structure in many research has the ability to inhibit acetylcholine esterase (AChE) enzyme and the ability of free radical scavenging.

We decided to design and synthesize a novel hybrid compound 5 (quinazoline- cinnamic acid) that supposed to have a dual biological activity to delay the progression of AD.

Synthesis of final hybrid compound was done through several reaction starting from N-methylisatoic anhydride which reacted with aqueous ammonia to form compound 2 with 90% yield.

Second step involved synthesis of spiro compound (3) with 90% yeild by reacted compound 2 with cyclopentanone.

Compound 4 was synthesized with 94% yield by reduction of compound 3 using LiAlH4 and compound 5 was synthesized in 46% of yield.

All reactions involved was monitored using TLC and GC-MS and characterized their final product by H-NMR and C-NMR.

In future, the hybrid compound 5 as potential drug candidate for AD could be biologically evaluated for its ability to inhibit AChE enzyme and its antioxidant activity

Main Topic

Pharmacology

Topics

No. of Pages

40

Table of Contents

Table of contents.

Abstract.

Abstract in Arabic.

Chapter One : Introduction.

Chapter Two : Review articles.

Chapter Three : Materials and method.

Chapter Four : Experimental.

Chapter Five : Results and discussion.

Chapter Six : Conclusions and recommendations.

References.

American Psychological Association (APA)

al-Ẓalimi, Duha Muhsin Abd al-Husayn. (2020). Synthesis and characterization of quinazoline-cinnamic acid hybrid as Alzheimer's drug candidate. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-988898

Modern Language Association (MLA)

al-Ẓalimi, Duha Muhsin Abd al-Husayn. Synthesis and characterization of quinazoline-cinnamic acid hybrid as Alzheimer's drug candidate. (Master's theses Theses and Dissertations Master). Isra University. (2020).
https://search.emarefa.net/detail/BIM-988898

American Medical Association (AMA)

al-Ẓalimi, Duha Muhsin Abd al-Husayn. (2020). Synthesis and characterization of quinazoline-cinnamic acid hybrid as Alzheimer's drug candidate. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-988898

Language

English

Data Type

Arab Theses

Record ID

BIM-988898